The present invention relates to the treatment of glaucoma and ocular hypertension. In particular, the present invention relates to the use of cloprostenol and fluprostenol analogues for the treatment of glaucoma and ocular hypertension.
Cloprostenol and fluprostenol, both known compounds, are synthetic analogues of PGF.sub.2.alpha., a naturally-occurring F-series prostaglandin (PG). Structures for PGF.sub.2.alpha. (I), cloprostenol (II), and fluprostenol (III), are shown below: ##STR1##
The chemical name for cloprostenol is 16-(3-chlorophenoxy)-17,18,19,20-tetranor PGF.sub.2.alpha.. Monograph No. 2397 (page 375) of The Merck Index, 11th Edition (1989) is incorporated herein by reference to the extent that it describes the preparation and known pharmacological profiles of cloprostenol. Fluprostenol has the chemical name 16-(3-trifluoromethylphenoxy)-17,18,19,20-tetranor PGF.sub.2.alpha.. Monograph No. 4121 (pages 656-657) of The Merck Index, 11th Edition (1989) is incorporated herein by reference to the extent that it describes the preparation and known pharmacological profiles of fluprostenol. Cloprostenol and fluprostenol are 16-aryloxy PGs and, in addition to the substituted aromatic ring, differ from the natural product PGF.sub.2.alpha. in that an oxygen atom is embedded within the lower (omega) chain. This oxygen interruption forms an ether functionality.
Naturally-occurring prostaglandins are known to lower intraocular pressure (lOP) after topical ocular instillation, but generally cause inflammation, as well as surface irritation characterized by conjunctival hyperemia and edema. Many synthetic prostaglandins have been observed to lower intraocular pressure, but such compounds also produce the aforementioned side effects which severely restrict clinical utility.